The leaves of Tridax procumbens were screened for the presence of bioactive molecules. They had high flavonoids, alkaloids, hydroxycinnamates, tannins and phytosterols, moderate benzoic acid derivatives and lignans, and low carotenoids contents. Thirty nine known alkaloids mainly akuammidine, 68.756%, twenty three known flavonoids mainly 17.593% kaempferol and 12.538% -epicatechin, five known carotenoids mainly lutein, 62.608%, four known benzoic acid derivatives mainly ferulic acid, 46.091%, two phytosterols mainly stigmasterol, 80.853% and six known lignans mainly galgravin, 77.326% were detected. Also detected were caffeic acid and tannic acid. The medicinal properties of the flavonoids, phytosterols, alkaloids, tannins, hydroxicinnamates, carotenoids, benzoic acid derivatives and lignans that were present in the leaves were discussed herein and proposed to be explored for their potential medicinal values. The great number of potentially active nutrients and their multifunctional properties make Tridax procumbens a perfect candidate for the production of health-promoting food and food supplements.